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Heterocyclic Amides: Inhibitors of Acyl-CoA:Cholesterol O -Acyl Transferase with Hypocholesterolemic Activity in Several Species and Antiatherosclerotic Activity in the Rabbit

โœ Scribed by White, Andrew D.; Purchase, Claude F.; Picard, Joseph A.; Anderson, Maureen K.; Bak Mueller, Sandra; Bocan, Thomas M. A.; Bousley, Richard F.; Hamelehle, Katherine L.; Krause, Brian R.; Lee, Peter; Stanfield, Richard L.; Reindel, James F.


Book ID
125832459
Publisher
American Chemical Society
Year
1996
Tongue
English
Weight
481 KB
Volume
39
Category
Article
ISSN
0022-2623

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The synthesis and structure-activity relationships of a series of malonester amide ACAT inhibitors are described. One of these compounds, 4s, was shown to be a potent inhibitor of both the intestinal and arterial enzymes, bioactive upon oral dosing (ex vivo bioassay) and efficacious in a clinically